Antiproliferative, cytotoxic and apoptotic activity of the bentonite transformation of sesquiterpene lactone glaucolide B to 5ß-hydroxy-hirsutinolide on tumor cell lines.

Numerous chemical compounds isolated from medicinal plants have anti-tumor properties, the effects of which on human cancer cells are currently under study. Here, the chemical transformation of glaucolide B were performed to produce a hirsutinolide. The antiproliferative and cytotoxic activity of 5ß-hydroxy-hirsutinolide and its ability to induce apoptosis in tumor and non-tumor cells (lymphocyte cultures and the normal HaCaT cell line) (1a) are reported. We ascertained that compound 1a exerts an inhibitory effect on the proliferation of SK-Lu-1, MDA-MB-231 and CaSki cells in a dose-dependent manner at IC50 values of 15, 18 and 30 µg/ml, respectively. The proliferation of lymphocyte cells treated with 1a was inhibited at a range from 14 to 28%, but the HaCaT cell line was not affected, suggesting that compound 1a has a selective action. Cytotoxic activity was evaluated by detecting the lactate dehydrogenase enzyme in supernatants from tumor and non-tumor cells. The 1a compound exhibited low or null cytotoxic activity in both cell types. The presence of apoptotic bodies and active caspase-3 in tumor cell lines treated with compound 1a are suggestive of apoptotic cell death. Notably, flow cytometry evaluation did not detect the presence of active caspase-3 on lymphocytes treated with this compound. Our results suggest that 5ß-hydroxy-hirsutinolide is a molecule with antiproliferative activity and low cytotoxic activity in tumor and non-tumor cells; this induces apoptotic cell death in tumor cell lines through selective action. Hence, this lactone could be considered a molecule worthy of study as an anti-tumor agent with therapeutic potential.

Quercetagetin and Patuletin: Antiproliferative, Necrotic and Apoptotic Activity in Tumor Cell Lines.

Quercetagetin and patuletin were extracted by the same method from two different Tagetes species that have multiple uses in folk medicine in Mexico and around the globe, one of which is as an anticancer agent. Their biological activity (IC50 and necrotic, apoptotic and selective activities of these flavonols) was evaluated and compared to that of quercetin, examining specifically the effects of C6 substitution among quercetin, quercetagetin and patuletin. We find that the presence of a methoxyl group in C6 enhances their potency.